Biofarmacia
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Examinando Biofarmacia por Asesores "Carpio Arevalo, Juan Marcelo"
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- ÍtemSolo MetadatosEstudio de Antraquinonas Sintéticas como Potenciales Inhibidores de la Enzima Beta-Glucuronidasa en Escherichia Coli(Universidad Católica de Cuenca., 2023) Guachichullca Espinoza, Karina Verónica.; Niguela Narvaez, Dayanna Valeria; Carpio Arevalo, Juan Marcelo; 0105782353; 0105782114The beta-glucuronidase enzyme of bacteria such as E. coli is responsible for adverse reactions at the intestinal level of some drugs used in chemotherapy, which causes some patients to abandon their treatments. For this reason, it is necessary to search for agents that can act as inhibitors of this enzyme. In this study we present the experimental results of the evaluation of the potential of synthetic anthraquinones in the inhibition of the enzyme beta-glucuronidase of E. coli, one of the most abundant species in the intestine. Under the conditions employed and at the concentrations tested anthraquinone, 1,8-dihydroxyanthraquinone, 1,2-dihydroxyanthraquinone, 1,5-dinitroanthraquinone, 1-chloroanthraquinone, 2-chloroanthraquinone, 1,8-dichloroanthraquinone, 1,5-dihydroxyanthraquinone, 1,5-dichloroanthraquinone, 1,8-dihydroxy-4,5-dinitroanthraquinone were not able to inhibit the activity of this enzyme. Furthermore, in silico toxicity predictions of each anthraquinone using the PROTOX-II program indicate that the compounds exhibit low hepatotoxic and cytotoxic potential, intermediate carcinogenic and immunogenic potential and high mutagenic potential. This study is a starting point for future research aimed at evaluating anthraquinones as potential inhibitors of the beta-glucuronidase enzyme of E. coli.
- ÍtemAcceso AbiertoEvolución del potencial antibacteriano y sinérgico de antraquinonas sintéticas sobre bacterias Gram-negativas resistentes a ciprofloxacina.(Universidad Católica de Cuenca., 2023) Cabrera Bermeo, Andrea Estefanía.; Vásquez Urgiles, Viviana Elizabeth; Carpio Arevalo, Juan Marcelo; 0107599532; 0107135543Antibiotics are used to treat bacterial diseases, but the emergence of resistant strains has become a global health problem. Anthraquinones are natural molecules with therapeutic effects. However, synthetic derivatives have been little studied. Objective: To evaluate the antibacterial effects of synthetic chlorinated, hydroxylated, and nitrated anthraquinones alone and combined with ciprofloxacin. Methods: The evaluation was performed on ciprofloxacin-resistant bacterial strains such as Escherichia coli and Klebsiella pneumoniae. Sensitivity to anthraquinones was evaluated by the Kirby-Bauer method using paper platelets. The macrodilution method in agar was used to determine MICs. Finally, bacteria were exposed to anthraquinones, and their effect was compared with the antibiotic without combination. Results: Information was provided on synthetic anthraquinones' antibacterial and synergistic capacity on ciprofloxacin-resistant bacteria, showing that anthraquinones had no antibacterial or synergistic effect on ciprofloxacin-resistant Klebsiella pneumoniae and Escherichia coli. However, 1,8-dihydroxy-4,5-dinitroanthraquinone showed the ability to increase the effect of ampicillin on Escherichia coli. Conclusion: This group of synthetic anthraquinones has expanded knowledge of the antibacterial potential. The hydroxyl, nitro, and chloride functional groups were also highlighted, indicating that none of the functional groups of anthraquinones have direct antibacterial activity. However, the combination of hydroxyl and nitro groups present in 1,8-dihydroxy-4,5-dinitroanthraquinone can increase the effect of ampicillin on Escherichia coli.